MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.

Product information

CAS Number: 1416581-40-2

Molecular Weight: 534.50

Formula: C27H26F4N2O5

Chemical Name: 3-{[(3aS,9R,9aR)-7-fluoro-4-[4-(trifluoromethoxy)benzoyl]-1H,2H,3H,3aH,4H,9H,9aH-cyclopenta[b]quinolin-9-yl](cyclopropyl)carbamoyl}propanoic acid

Smiles: OC(=O)CCC(=O)N([C@@H]1[C@@H]2CCC[C@@H]2N(C2=CC=C(F)C=C21)C(=O)C1C=CC(=CC=1)OC(F)(F)F)C1CC1

InChiKey: BNMORDXQPYWZBW-FZOAFFARSA-N

InChi: InChI=1S/C27H26F4N2O5/c28-16-6-11-22-20(14-16)25(32(17-7-8-17)23(34)12-13-24(35)36)19-2-1-3-21(19)33(22)26(37)15-4-9-18(10-5-15)38-27(29,30)31/h4-6,9-11,14,17,19,21,25H,1-3,7-8,12-13H2,(H,35,36)/t19-,21+,25-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

MK-8318 also inhibits β-arrestin, cAMP, CYP3A4, CYP2C9, and CYP2D6 with IC50s of 3.5±2.1 nM, 8.0±6.8 nM, 50 µM, 50 µM and 50 µM.

In Vivo:

In a sheep model, MK-8318 blocks late airway response (LAR) and airway hyperresponsiveness (AHR) after i.v. infusion at 1 mg/kg. MK-8318 shows 76% LAR efficacy and 114% AHR efficacy. MK-8318 also displays good efficacy on BAL cells/pulmonary function from ovalbumin sensitized and challenged Brown Norway rats at 3, 10, and 30 mg/kg oral dosing.

Products are for research use only. Not for human use.